Discover : Two kinds of compounds can block HIV virus particle and take shape

Discover : Two kinds of compounds can block HIV virus particle and take shape

According to report on February 3 of American Scripps research institute website, scientist should find two kinds of compounds recently, can act on HIV (HIV) The new combination position of protease, thus has established the foundation for developing curative effect and resisting the new AIDS medicine able to bear nature better. It is here that the relevant research results will be published Publish in March >On the magazine .
Protease inhibitor is one of the medicines used in AIDS treatment extensively. Generally, the shape of HIV protease will show its function. In duplicate in the course oneself, virus will make one long the intersection of albumen and chain, and protease will crack for short passage their, in order to make the new HIV virus particle assemble success finally.
Both sides of protease molecule grow wing flap of kind of two scissors, finish isolating the task of the passage from long albumen chain by the opening and closing of wing flap. Present HIV protease medicine, that is that imitates some areas of HIV protease chain (if click in the cracked location) Shape,not ordering to tie definitely location of and protease positions hollow, thus make protease not lasted efficiency, prevent HIV from producing the new infection particle.
Arthur, Allson of Scripps research institute research assistant Alex L Perryman in the laboratory, use the computer to a variation HIV poisonous one (V82F/I84V) with multiple drug resistance Sport state go on imitate . The result shows, the wing flap against nature protease molecule will be opened more more than the wing flap of the ordinary protease molecule, and more flexible. Enter active location, order, tie definitely at the groove as medicine, want, close wing flap, need more energy, but the present medicine can't offer the energy . Result its whether medicine can remain in, tie, make a reservation some, groove will use the intersection of HIV and the intersection of albumen and chain, thus produced the new infection particle.
Through imitating the experiment, Perryman and colleague have confirmed the method to solve this problem. Like control scissors open and close, need on the scissors handle the application of force, Perryman imagines, new medicine should be able to order, tie, definitely, inhibit the wing flap from from the end with the intersection of protease and available location of both sides, give and resist HIV medicine to close the wing flap by enough help, make protease fail. These compounds should be one kind " L Turn into and construct the passage " ,Have small molecular structure, can change the mechanics characteristic of the molecule.
In order to find this kind of compound, in the past several years, Perryman research group has screened to several hundred compound passages. They different conformation in molecule carry on, take treatment while being brilliant at first, then select a group of passages from the crystal, pass the synchronous radiation light source (SSRL) of Stamford To judge any one have structure characteristics needed in them. Finally, researchers have found two sample - -Passage 2- Methyl surrounds ethanol and indole - 6- Carboxyl acid . Verify passage these really can order, tie definitely with new location of protease through additional the intersection of x and the intersection of ray and crystalline experiment, thus will change the structure of protease to have a partiality for.
Assistant professor C Davies of Scripps research institute holds and refers in particular to happen, this research can make the scientist spy upon a brand-new medicine design method to oppose HIV protease. Studies have suggested protease molecule have two non- active location order, tie the groove (and construct the position) definitely ,Can be used for developing the face-off HIV new strategy which is able to bear nature.
Perryman claims, the experiment has verified that calculates the model is supposed, namely HIV protease gets rid of the surface groove clicked in active location, can tie the medicine definitely. Can make present active some location inhibit medicine from to be effective with the some for medicine that target order. And it is effective to regard some of non- active location as the mark strategy of medicine to other diseases, especially even more like this when there is gene mutation to lead to the fact drug resistance appears. Two new compound these very small, " L The passage " ,So can't expect them to become strong inhibitor yet at present. But this is a beginning, Perryman says, this result of study is laid a structural foundation for developing new resisting AIDS medicine. (Liu HaiYing ) (Source : Science and Technology Daily )
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